Evidence map›Paper›PMID 31790916›Full record

ArticleJournal of chromatography. B, Analytical technologies in the biomedical and life sciences2019

Bioanalytical method development and validation of MES207, a neuropeptide FF receptor antagonist, and its application in preclinical pharmacokinetics.

Tamara I King, Ann-Cathrin Roewekamp, Abhisheak Sharma, Sydney Harrison, Christophe Mesangeau, Marco Mottinelli, Shyam H Kamble, Christopher R McCurdy, Bonnie A Avery

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact, top 80% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 2 institutions in 1 country.

Tamara I KingDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA; Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Ann-Cathrin RoewekampDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA.
Abhisheak SharmaDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA; Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Sydney HarrisonDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA; Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Christophe MesangeauDepartment of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Marco MottinelliDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA; Department of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Shyam H KambleDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA.
Christopher R McCurdyDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA; Department of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA. Electronic address: cmccurdy@cop.ufl.edu.
Bonnie A AveryDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA; Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
University of Florida · USUniversity of Mississippi · US

Funding

Center of Research Excellence in Natural Products Neuroscience (CORE-NPN)P20GM104932 · NIGMS · UNIVERSITY OF MISSISSIPPI · PI MAJUMDAR, SOUMYAJIT · 2012 to 2016
$10.0M
Kratom alkaloids: in vitro and in vivo pharmacological mechanismsR01DA047855 · NIDA · UNIVERSITY OF FLORIDA · PI MCCURDY, CHRISTOPHER R, MCMAHON, LANCE R. · 2019 to 2023
$3.6M
Optimization of non-peptide probes for the NPFF receptor systemR01DA034777 · NIDA · UNIVERSITY OF MISSISSIPPI · PI MCCURDY, CHRISTOPHER R · 2014 to 2016
$1.5M
NIDA NIH HHS R01 DA034777NIDA NIH HHS R01 DA047855NIGMS NIH HHS P20 GM104932
6 · The paper itself

Abstract

The nonpeptide small molecule, MES207, exhibits 17-fold preferential binding to the neuropeptide FF receptor 1 (NPFFR1) over NPFFR2 and shows antagonist functionality at NPFF receptors. In order to further the development of MES207 as a NPFFR1 probe, an UPLC-MS/MS bioanalytical method was developed and validated to quantify MES207 in rat plasma for a linearity range of 3-200 ng/mL. The method was applied in the analysis of the plasma, brain, and urine samples collected during pharmacokinetic studies in healthy male and female Sprague Dawley rats. The animals were dosed through oral gavage (50 mg/kg) and intravenously (2.5 mg/kg). Test samples were analyzed using the validated bioanalytical method to generate plasma concentration-time profiles. The results were further subjected to non-compartmental analysis using Phoenix 6.4®. MES207 exhibits a large volume of distribution (1.2 ± 0.6 L), high clearance (0.8 ± 0.1 L/h), and a poor oral bioavailability (1.7 ± 0.4%). The compound also showed a multiple peak phenomenon with a very short absorption phase. It appears that gender does not significantly influence the differences in pharmacokinetic parameters of this NPFF probe.

Indexed as

AnimalsChromatography, High Pressure LiquidDrug StabilityFemaleGuanidinesLimit of DetectionLinear ModelsMalePiperidinesRatsRats, Sprague-DawleyReceptors, NeuropeptideReproducibility of ResultsTandem Mass Spectrometry1-benzyl-N-(2-guanidinoethyl)-4-(phenylamino)piperidine-4-carboxamideGuanidinesneuropeptide FF receptorPiperidinesReceptors, NeuropeptideMES207NPFF antagonistPharmacokineticsUPLC-MS/MS

Identifiers

PMID31790916
PMCPMC7027589
OpenAlexW2986919800

What OpenQuestion holds

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LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.